20158-69-4Relevant academic research and scientific papers
STAT3 DIMERIZATION INHIBITORS
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Page/Page column 41; 42, (2014/05/24)
The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as wel
Development of new N-arylbenzamides as STAT3 dimerization inhibitors
Urlam, Murali K.,Pireddu, Roberta,Ge, Yiyu,Zhang, Xiaolei,Sun, Ying,Lawrence, Harshani R.,Guida, Wayne C.,Sebti, Said M.,Lawrence, Nicholas J.
, p. 932 - 941 (2013/07/27)
The O-tosylsalicylamide S3I-201 (10) was used as a starting point for design and synthesis of novel STAT-3 dimerization inhibitors with improved drug-like qualities. The phosphonic acid 12d and salicylic acids 13f, 13g with a shorter amide linker lacking
Progresses in the pursuit of aldose reductase inhibitors: The structure-based lead optimization step
Ramunno, Anna,Cosconati, Sandro,Sartini, Stefania,Maglio, Vita,Angiuoli, Sara,La Pietra, Valeria,Di Maro, Salvatore,Giustiniano, Mariateresa,La Motta, Concettina,Da Settimo, Federico,Marinelli, Luciana,Novellino, Ettore
, p. 216 - 226 (2012/07/16)
Aldose reductase (ALR2) is a crucial enzyme in the development of the major complications of diabetes mellitus. Very recently it has been demonstrated that the ARL2 inhibitor, fidarestat, significantly prevents inflammatory signals (TNF-α, LPS) that cause cancer (colon, breast, prostate and lung), metastasis, asthma, and other inflammatory diseases. Currently, fidarestat is in phase III clinical trial for diabetic neuropathy and was found to be safe. Thus the finding of novel, potent ARL2 inhibitors is today more than in the past in great demand as they can pave the way for a novel therapeutic approach for a number of diseases besides the diabetes. Herein, starting from the virtual screening-derived ALR2 inhibitor S12728 (1), a rational receptor-based lead optimization has been undertaken. The design and synthetic efforts here reported led to the discovery of several new compounds endowed with low micromolar/submicromolar activities.
HIV protease inhibitors based on amino acid derivatives
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, (2008/06/13)
A compound selected from the group consisting of a compound of formula I 1a compound of formula II 2and when the compound of formula I and II comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein R1, R2, Cx, n, R3, R4, R5, Y are as defined in the specification.
Protease inhibitors - Part 5. Alkyl/arylsulfonyl- and arylsulfonylureido-/arylureido- glycine hydroxamate inhibitors of Clostridium histolyticum collagenase
Scozzafava, Andrea,Supuran, Claudiu T.
, p. 299 - 307 (2007/10/03)
Reaction of alkyl/arylsulfonyl halides with glycine afforded a series of derivatives which were first N-benzylated by treatment with benzyl chloride, and then converted to the corresponding hydroxamic acids with hydroxylamine in the presence of carbodiimide derivatives. Other derivatives were obtained by reaction of N-benzyl-glycine with aryl isocyanates, arylsulfonyl isocyanates or benzoyl isothiocyanate, followed by conversion of their COOH group into the CONHOH moiety, as mentioned above. The 90 new compounds reported here were assayed as inhibitors of the Clostridium histolyticum collagenase (EC 3.4.24.3), a zinc enzyme which degrades triple helical regions of native collagen. The prepared hydroxamate derivatives were generally 100-500 times more active than the corresponding carboxylates. In the series of synthesized hydroxamates, substitution patterns leading to the best inhibitors were those involving perfluoroalkylsulfonyl- and substituted- arylsulfonyl moieties, such as pentafluorophenylsulfonyl, 3- and 4- carboxyphenylsulfonyl-, 3-trifluoromethyl-phenylsulfonyl or 1- and 2-naphthyl among others. Thus, it seems that similarly to the matrix metalloproteinase (MMP) hydroxamate inhibitors, Clostridium histolyticum collagenase inhibitors should incorporate hydrophobic moieties at the P1, and P2, sites, whereas the α-carbon substituent may be a small and compact moiety (such as H. for the Gly derivatives reported here). Such compounds might lead to the design of collagenase inhibitor-based drugs useful as anti-cancer, anti-arthritis or anti-bacterial agents for the treatment of corneal keratitis. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents
Caldarelli, Marina,Habermann, Joerg,Steven V, Ley
, p. 2049 - 2052 (2007/10/03)
Polymer-supported reagents and sequestering agents may be used to generate an array of variously substituted hydroxamic acid derivatives as potential inhibitors of matrix metalloproteinases without any chromatographic purification step.
Solid Phase Synthesis of N-Alkyl Sulfonamides
Dankwardt, Sharon M.,Smith, David B.,Porco Jr., John A.,Nguyen, Cindy H.
, p. 854 - 856 (2007/10/03)
Polymer-supported sulfonamides were alkylated using alkyl halides in the presence of DBU or with alcohols via the Mitsunobu reaction.
BENZOPHENANTHRIDINES. VIII. SYNTHESIS AND STRUCTURE OF cis-2-METHOXY-5-TOSYL-4b,5,6,10b,11,12-HEXAHYDROBENZOPHENANTHRIDINE
Rozhkov, V. S.,Sladkov, V. I.,Turdybekov, K. M.,Lindeman, S. V.,Kolesnikov, A. Yu.,et al.
, p. 1162 - 1167 (2007/10/02)
The total synthesis of cis-2-methoxy-5-tosyl-4b,5,6,10b,11,12-hexahydrobenzophenathridine was realized from the hydrochloride of methyl aminoacetate by successive ring growth AB->ABD->ABDC in five stages, including the addition of 3-methoxyphenylmagnes
